PCL201H1 Study Guide - Final Guide: Fluoxetine, Antiarrhythmic Agent, Propafenone
7 Apr 2016
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Reaction/importance of it imp in drug-drug interactions and bioavailability(due to wide range of substrate types/competition) Metabolize ~50% of known drugs (ex/ erythromycin, codeine, lovastatin, diazepam, taxol) Btfs caffeine acetaminophen aromatic amine carcinogens, aflatoxin (a liver carcinogen) Esp major p450 in human fetal liver. Can be induced by wide range of xenobiotics. Expressed in human liver but not in human extrahepatic tissues. Induced by polycyclic aromatic hydrocarbons (ex/ pahs in cigarette smoke) Cyp1a1(prof"s favourite): close relative of 1a2 , widely expressed in tissues other than liver; no appreciable level in human level; can also be induced by pah, causing lung cancer. Polymorphic in human (slow or fast phenotypes in diff individuals) Highly polymorphic (imp)>highly various drug metabolism in ppl. Small a. site, focus on small molecules, similar in size of oh and benzene. **=important; btf=biotransformation: tolbutaminde (hypoglycemic agent, phenytoin (anticonvulsant), **warfarin (anticoagulant; also polymorphic> dosage adjustment required)
